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Open AccessArticle

Acetal-Linked Paclitaxel Polymeric Prodrug Based on Functionalized mPEG-PCL Diblock Polymer for pH-Triggered Drug Delivery

by Yinglei Zhai 1,2,†, Xing Zhou 3,†, Lina Jia 4, Chao Ma 5, Ronghua Song 1, Yanhao Deng 1, Xueyao Hu 1 and Wei Sun 1,*
Department of Biomedical Engineering, School of Medical Devices, Shenyang Pharmaceutical University, Shenyang 110016, China
State Key Laboratory for Marine Corrosion and Protection, Luoyang Ship Material Research Institute (LSMRI), Qingdao 266101, China
Hainan Institute of Materia Medica, Haikou 570311, China
Department of Pharmacology, School of Life Science and Biopharmaceutics, Shenyang Pharmaceutical University, Shenyang 110016, China
College of Food & Pharmaceutical Engineering, Guizhou Institute of Technology, Guizhou 550003, China
Author to whom correspondence should be addressed.
These two authors contributed equally to this work
Polymers 2017, 9(12), 698;
Received: 14 October 2017 / Revised: 17 November 2017 / Accepted: 7 December 2017 / Published: 11 December 2017
(This article belongs to the Special Issue Polymer Micelles)
The differences in micro-environment between cancer cells and the normal ones offer the possibility to develop stimuli-responsive drug-delivery systems for overcoming the drawbacks in the clinical use of anticancer drugs, such as paclitaxel, doxorubicin, and etc. Hence, we developed a novel endosomal pH-sensitive paclitaxel (PTX) prodrug micelles based on functionalized poly(ethylene glycol)-poly(ε-caprolactone) (mPEG-PCL) diblock polymer with an acid-cleavable acetal (Ace) linkage (mPEG-PCL-Ace-PTX). The mPEG-PCL-Ace-PTX5 with a high drug content of 23.5 wt % was self-assembled in phosphate buffer (pH 7.4, 10 mM) into nanosized micelles with an average diameter of 68.5 nm. The in vitro release studies demonstrated that mPEG-PCL-Ace-PTX5 micelles was highly pH-sensitive, in which 16.8%, 32.8%, and 48.2% of parent free PTX was released from mPEG-PCL-Ace-PTX5 micelles in 48 h at pH 7.4, 6.0, and 5.0, respectively. Thiazolyl Blue Tetrazolium Bromide (MTT) assays suggested that the pH-sensitive PTX prodrug micelles displayed higher therapeutic efficacy against MCF-7 cells compared with free PTX. Therefore, the PTX prodrug micelles with acetal bond may offer a promising strategy for cancer therapy. View Full-Text
Keywords: prodrug; polymer micelles; pH-sensitive; acetal; paclitaxel prodrug; polymer micelles; pH-sensitive; acetal; paclitaxel
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MDPI and ACS Style

Zhai, Y.; Zhou, X.; Jia, L.; Ma, C.; Song, R.; Deng, Y.; Hu, X.; Sun, W. Acetal-Linked Paclitaxel Polymeric Prodrug Based on Functionalized mPEG-PCL Diblock Polymer for pH-Triggered Drug Delivery. Polymers 2017, 9, 698.

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